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Ligands (Drugs)
Definitions Classification
Ligand-Receptor interaction
Interaction and consequence Receptor-mediated mechanism of action
Drug Receptors
Receptor: Definitions
Synonym: Target molecule Macromolecule (or macromolecular complex)
which binds agonists with high structural selectivity with the consequence that a characteristic effect occurs
Or site of drug action responsible for the pharmacological effect The component of the organism with which the chemical agent was presumed
to interact.
organism
Types of Binding
Reversible
bonds Slowly reversible /irreversible high affinity non-covalent binding, covalent binding
Differences between
Specific Receptors and Non-specific Drug Targets
Specific receptors
are stereoselective can be selectively blocked by
as Ligands.
Ligands are classified into 2 groups Agonist: molecule that binds to receptor and produces similar response to
that of the endogenous ligand
Partial agonist agonist that produce partial effect
the receptor.
high affinity: low concentrations bind low affinity: high concentrations bind
no affinity:
Efficacy: the intrinsic activity Max. effect efficacy = 1 Min. effect efficacy = 0
Location
Consequence of interaction Secondary chemical messenger involved in the transduction
pathway Etc.
Based on Location
Example 1 Receptors of the nervous system Post-synaptic receptor Pre-synaptic receptor
Example 2 Receptors that are on the surface and inside the cells Cell-surface receptor
Ion-channel-linked receptors G-protein-linked receptors Enzyme-linked receptors Intracellular receptor
different kinds and can be used to classify the receptors connected to them.
Drug Cyclic AMP Cyclic GMP Phosphoinositol Arachidonic acid Calcium ion
Receptors
Effector or Target
Drug-Receptor Interaction
Structure specific
Drug + Receptor
Affinity
Stereo-selective
Lock and key mechanism
Drug-receptor complex
Transduction pathways
Response
Efficacy Potency
beneficial effect caused by the drugs ability to interact with the receptor and change
physiological
or biochemical
or pathological processes
Drug
Binding Site
intermediate messengers e.g. cyclic AMP
Effect
Mechanism of action
Classical Receptors
Drug actions on Classical receptors are based on types of Ligands
Agonist
receptor
action
receptor
receptor
action
action
Mechanism of action
Uptake Carriers
Uptake carriers or Transport proteins
can have a role in regulation of drug action Example: Norepinephrine (NE) action
Drug
Uptake inactivation
NE
X
NE release from nerve
More NE
Receptors Increase NE action Neurotransmission
Rapid inactivation
Decrease NE action
Mechanism of action
Enzymes
drug-enzyme interaction
Action of Neostigmine
Somatic Nervous System (voluntary)
N Nicotinic ACh
receptor
ACh
N
N
AChE
Skeletal Muscle
N
Neostigmine
acetate choline
Arachidonic Acid
(released from cell membrane) Cyclooxygenase (COX)
Action of Aspirin
Infection
Cyclooxygenase
Prostaglandins
Aspirin
Pain
Fever